同义名 : | - | |
CAS号 : | 70006-24-5 | |
货号 : | A1000642 | |
分子式 : | C17H19N5 | |
纯度 : | 98%+ | |
分子量 : | 293.366 | |
MDL号 : | MFCD05262347 | |
存储条件: |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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描述 | Dopamine is the main catecholamine in the central nervous system. The dopamine D4 receptor is abundantly expressed in the cortex and hypothalamus, and plays a key role in the regulation of sexual function in mammals. ABT-724 is a highly potent, selective dopamine D4 receptor with an EC50 value of 12.4nM and 61% efficacy for human dopamine D4 receptor, but shows no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 also exhibits potent but partial agonist effects on rat and ferret D4 receptors with EC50 values of 14.3±0.6nM and 23.2±1.3nM, respectively. Subcutaneous injection of ABT-724 at doses of 0.01, 0.03, 0.1, 0.3, and 1μmol/kg induced significant facilitation of penile erection in rats. The maximal effect was observed at 0.03μmol/kg with a 77% incidence, compared to 23% incidence in the control group. The latency to induce a penile erection in ABT-724-treated rats was 18.7 minutes. Also in rats with chronically implanted cannulas, injection of ABT-724 directly into the lateral ventricle significantly facilitated erectile responses at 3nmol. Subcutaneous administration of ABT-724 at 0.0025μmol/kg resulted in 2.0±0.6 episodes of increase in intracavernous pressure in an awake freely moving rat.[1] | ||
作用机制 | ABT-724 is a selective dopamine D4 receptor agonist that facilitates penile erection in rats without affecting cardiovascular, gastrointestinal, or central nervous system function.[1] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.41mL 0.68mL 0.34mL |
17.04mL 3.41mL 1.70mL |
34.09mL 6.82mL 3.41mL |
参考文献 |
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